tcsc0287 Cinacalcet

Cinacalcet is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.

In Vivo: Cinacalcet HCl (5 and 10 mg/kg) results in a significant reduction in parathyroid gland weight in 5/6 nephrectomy animals. In sham animals, Cinacalcet HCl has no effect on parathyroid gland cell proliferation or parathyroid weight compared with vehicle treatment. There are no differences in serum phosphorus levels in Cinacalcet HCl (10, 5, or 1 mg/kg) treated 5/6 nephrectomized animals compared with vehicle-treated 5/6 nephrectomized animals. Cinacalcet HCl treatment significantly reduces blood ionized calcium levels in sham animals^[1]. Cinacalcet (30 mg/kg/24 h) leads to a marked reduction in circulating parathyroid hormone and a modest reduction in serum Ca. Cinacalcet does not alter UCa when the GHS rats are fed the normal Ca diet but lowers UCa when they are fed the low Ca diet. Cinacalcet does not alter U supersaturation with respect to either CaOx or CaHPO4 on either diet^[2].